Description
Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR) receptor tyrosine kinase. It inhibits EGFR L858R/T790M double mutations with an IC₅₀ value of 0.18 nM which is nearly 43-fold potent over wild-type EGFR (IC₅₀ value of 7.68 nM) in kinase assays. In a xenograft model, oral administration at a daily dose of 500 mg/kg results in complete remission of tumors with EGFR-active and T790M mutations.
Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR) receptor tyrosine kinase. It inhibits EGFR L858R/T790M double mutations with an IC₅₀ value of 0.18 nM which is nearly 43-fold potent over wild-type EGFR (IC₅₀ value of 7.68 nM) in kinase assays. In a xenograft model, oral administration at a daily dose of 500 mg/kg results in complete remission of tumors with EGFR-active and T790M mutations.
Alternate Name/Synonyms: Abivertinib; N-[3-[[2-[3-fluoro-4-(4-methylpiperazin-1-yl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]phenyl]prop-2-enamide; N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide; AC0010
Appearance: White to off-White Powder
Formulation:
CAS Number: 1557267-42-1
Structure Available?: True
Peptide sequence:
Salt Form: False
Molecular Formula: C₂₆H₂₆FN₇O₂
Molecular Weight: 487.53
Cell-Permeable?: False
Purity: >98%
Solubilities: ~30 mg/ml in DMSO, ethanol, DMF
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Country of Origin: USA
Tag Line: An irreversible EGFR inhibitor
MDL Number: MFCD29089376
PubChem CID: 72734520
SMILES: CN1CCN(CC1)C2=C(C=C(C=C2)NC3=NC4=C(C=CN4)C(=N3)OC5=CC=CC(=C5)NC(=O)C=C)F
InChi: InChI=1S/C26H26FN7O2/c1-3-23(35)29-17-5-4-6-19(15-17)36-25-20-9-10-28-24(20)31-26(32-25)30-18-7-8-22(21(27)16-18)34-13-11-33(2)12-14-34/h3-10,15-16H,1,11-14H2,2H3,(H,29,35)(H2,28,30,31,32)
InChi Key: UOFYSRZSLXWIQB-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20ºC |
Shipping Condition: |
RT |
Shelf Life: |
36 months |